US2017000767A1PendingUtilityA1

Therapeutic or prophylactic agent for multiple sclerosis

Assignee: TORAY INDUSTRIESPriority: Jan 29, 2014Filed: Jan 29, 2015Published: Jan 5, 2017
Est. expiryJan 29, 2034(~7.5 yrs left)· nominal 20-yr term from priority
A61P 25/28A61P 25/00A61K 31/415A61K 31/421A61K 31/4439A61K 31/426A61K 9/0053
30
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Claims

Abstract

A therapeutic or prophylactic agent for multiple sclerosis includes as an effective component a cyclohexane derivative represented by Formula (I): wherein A is a substituent represented by Formula (IIa) or (IIb): R 1 and R 2 are each independently a hydrogen atom, chlorine atom, C 1 -C 3 haloalkyl, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or cyano; R 3 is a hydrogen atom or chlorine atom; R 4 is a fluorine atom, hydroxymethyl, or hydroxyl; R 5 and R 6 are each independently a hydrogen atom, fluorine atom, C 1 -C 3 haloalkyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, C 1 -C 4 alkoxy, hydroxyl, or C 2 -C 5 alkylcarbonyloxy, or optionally together form oxo; R 7 and R 8 are each independently a hydrogen atom or fluorine atom; Y is an oxygen atom or sulfur atom; and Z is a nitrogen atom or methane or a pharmaceutically acceptable salt thereof.

Claims

exact text as granted — not AI-modified
1 - 6 . (canceled) 
     
     
         7 . A therapeutic or prophylactic agent for multiple sclerosis, comprising, as an effective component, a cyclohexane derivative represented by Formula (I): 
       
         
           
           
               
               
           
         
       
       wherein
 A is a substituent represented by Formula (IIa) or (IIb): 
 
       
         
           
           
               
               
           
         
         R 1  and R 2  are each independently a hydrogen atom, chlorine atom, C 1 -C 3  haloalkyl, C 1 -C 4  alkyl, C 1 -C 4  alkoxy, or cyano; 
         R 3  is a hydrogen atom or chlorine atom; 
         R 4  is a fluorine atom, hydroxymethyl, or hydroxyl; 
         R 5  and R 6  are each independently a hydrogen atom, fluorine atom, C 1 -C 3  haloalkyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, C 1 -C 4  alkoxy, hydroxyl, or C 2 -C 5  alkylcarbonyloxy, or optionally together form oxo; 
         R 7  and R 8  are each independently a hydrogen atom or fluorine atom; 
         Y is an oxygen atom or sulfur atom; and 
         Z is a nitrogen atom or methane 
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         8 . A therapeutic or prophylactic agent for multiple sclerosis, comprising, as an effective component, a cyclohexane derivative represented by Formula (I): 
       
         
           
           
               
               
           
         
       
       wherein
 A is a substituent represented by Formula (IIc) or (IId): 
 
       
         
           
           
               
               
           
         
         R 1  and R 2  are each independently a hydrogen atom, chlorine atom, C 1 -C 3  haloalkyl, C 1 -C 4  alkyl, or C 1 -C 4  alkoxy; 
         R 3  is a hydrogen atom or chlorine atom; 
         R 4  is a fluorine atom, hydroxymethyl, or hydroxyl; 
         R 5  and R 6  are each independently a hydrogen atom, fluorine atom, C 1 -C 3  haloalkyl, carboxyl, C 1 -C 4  alkoxy, hydroxyl, or C 2 -C 5  alkylcarbonyloxy, or optionally together form oxo; 
         Y is an oxygen atom or sulfur atom; and 
         Z is a nitrogen atom or methane 
       
       or a pharmaceutically acceptable salt thereof. 
     
     
         9 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 7 , wherein R 1  and R 2  are each independently trifluoromethyl, methyl, or methoxy. 
     
     
         10 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 7 , wherein R 3  is a hydrogen atom. 
     
     
         11 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 7 , wherein R 4  is hydroxymethyl or hydroxyl. 
     
     
         12 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 7 , wherein R 3  and R 6  are each independently a hydrogen atom, fluorine atom, trifluoromethyl, carboxyl, methoxy, hydroxyl, or acetyloxy, or optionally together form oxo. 
     
     
         13 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 8 , wherein R 1  and R 2  are each independently trifluoromethyl, methyl, or methoxy. 
     
     
         14 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 8 , wherein R 3  is a hydrogen atom. 
     
     
         15 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 9 , wherein R 3  is a hydrogen atom. 
     
     
         16 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 8 , wherein R 4  is hydroxymethyl or hydroxyl. 
     
     
         17 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 9 , wherein R 4  is hydroxymethyl or hydroxyl. 
     
     
         18 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 10 , wherein R 4  is hydroxymethyl or hydroxyl. 
     
     
         19 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 8 , wherein R 5  and R 6  are each independently a hydrogen atom, fluorine atom, trifluoromethyl, carboxyl, methoxy, hydroxyl, or acetyloxy, or optionally together form oxo. 
     
     
         20 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 9 , wherein R 5  and R 6  are each independently a hydrogen atom, fluorine atom, trifluoromethyl, carboxyl, methoxy, hydroxyl, or acetyloxy, or optionally together form oxo. 
     
     
         21 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 10 , wherein R 5  and R 6  are each independently a hydrogen atom, fluorine atom, trifluoromethyl, carboxyl, methoxy, hydroxyl, or acetyloxy, or optionally together form oxo. 
     
     
         22 . The therapeutic or prophylactic agent for multiple sclerosis according to  claim 11 , wherein R 5  and R 6  are each independently a hydrogen atom, fluorine atom, trifluoromethyl, carboxyl, methoxy, hydroxyl, or acetyloxy, or optionally together form oxo.

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